米那普明可拮抗三氟甲基苯基哌嗪（TFMPP）对乙酰胆碱释放的血清素能抑制作用。

Minaprine antagonises the serotonergic inhibitory effect of trifluoromethylphenylpiperazine (TFMPP) on acetylcholine release.

作者信息

Bolanos F, Fillion G

机构信息

Unité de Pharmacologie Neuro-Immuno-Endocrinienne de l'Institut Pasteur, Paris, France.

出版信息

Eur J Pharmacol. 1989 Sep 1;168(1):87-92. doi: 10.1016/0014-2999(89)90636-5.

DOI:10.1016/0014-2999(89)90636-5

PMID:2583235

Abstract

The serotonin agonist, m-trifluoromethylphenylpiperazine (TFMPP), inhibited the K+-evoked release of [3H]acetylcholine ([3H]ACh) from rat hippocampal synaptosomes. The inhibitory effect of TFMPP was blocked by the non-selective 5-HT1 antagonist, methiothepin, but was not affected by ketanserin, mesulergine or spiperone. The 5-HT3 antagonist, MDL 72222, slightly reversed the inhibitory effect. The antidepressant, minaprine, did not modify the basal release of [3H]ACh but it antagonised the inhibitory effect of TFMPP on the K+-evoked release. The maximal reversal was found at 0.3 microM minaprine. These results suggest that minaprine interacts with heterologous presynaptic 5-HT1B receptors. A new approach is thus opened to the study of the mechanism of action of antidepressant drugs.

摘要

血清素激动剂间三氟甲基苯基哌嗪（TFMPP）抑制了钾离子诱发的大鼠海马突触体中[³H]乙酰胆碱（[³H]ACh）的释放。TFMPP的抑制作用可被非选择性5-羟色胺1拮抗剂美噻吨阻断，但不受酮色林、甲磺麦角新碱或螺哌隆影响。5-羟色胺3拮抗剂MDL 72222可轻微逆转这种抑制作用。抗抑郁药米那普明不会改变[³H]ACh的基础释放，但它能拮抗TFMPP对钾离子诱发释放的抑制作用。在0.3微摩尔/升米那普明时发现最大逆转作用。这些结果表明米那普明与异源突触前5-羟色胺1B受体相互作用。因此，为抗抑郁药物作用机制的研究开辟了一条新途径。